A 419259
Based on 12 publication(s) in Google Scholar
A 419259 is a broad-spectrum pyrrolo-pyrimidine inhibitor, has high selectivity towards the Src family. A 419259 shows inhibitory effect for Src, Lck and Lyn with IC50 of 9 nM, <3 nM and <3 nM, respectively.
For research use only. We do not sell to patients.
- Purity : 99.88%
- CAS No.: 364042-47-7
- Formula: C29H34N6O
- Molecular Weight:482.63
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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A 419259 (GMP)Src Inhibitor
Publications Citing Use of MedChemExpress (MCE) A 419259
More- Blood. 2016 Jun 23;127(25):3237-52. [Abstract]
- Adv Sci (Weinh). 2025 Jun 30:e17764. [Abstract]
- Clin Transl Med. 2026 Jul;16(7):e70731.
- Aging Cell. 2026 Jan 20;25(2):e70352.
- J Med Chem. 2024 Nov 28;67(22):20571-20579. [Abstract]
- Commun Biol. 2026 Apr 9;9(1):780. [Abstract]
- Microb Pathog. 2025 Feb:199:107252. [Abstract]
- Biochem Biophys Res Commun. 2026 Aug 27:828:154112. [Abstract]
- Res Sq. 2026 May 8:rs.3.rs-9500406. [Abstract]
- Free University of Berlin. 2025 Aug 4.
- Patent. US20250228856A1.
- Patent. US20170333436A1.
Biological Activity
Description
IC50 & Target
IC50: 9 nM (Src), <3 nM (Lck), <3 nM (Lyn), 3 μM (Abl)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MV4-11 | GI50 |
40 nM
Compound: RK-20449
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Growth inhibition of human MV4-11 cells after 3 days by Alamar blue assay
Growth inhibition of human MV4-11 cells after 3 days by Alamar blue assay
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[PMID: 29037944] |
In Vitro
"A419259 is a second-generation pyrrolopyrimidine that blocks proliferation and induces apoptosis in CML cell lines. It induces apoptosis in K-562 cells and also inhibits Meg-01 proliferation (IC50=0.1 μM)[1].
In the absence of IL-3, A-419259 strongly inhibits DAGM/Bcr-Abl cell proliferation (IC50=0.1-0.3 μM)[1].
A-419259 also inhibits overall SFK activity in CML cell lines and blocks Src kinase activation (IC50=0.1-0.3 μM)[1].
A 419259 (1 μM; 16 h) inhibits endogenous SFK (c-Src and Lck) activity, thereby inhibiting Src-driven differentiation of mES cells toward primitive ectoderm-like cells[2].
A 419259 (0.3, 1 μM; 5 days) has no effect on undifferentiated colony morphology of hES cells grown in mTeSR medium[2].
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MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 364042-47-7
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Appearance Solid
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Molecular Weight 482.63
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Formula C29H34N6O
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Color White to light yellow
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SMILES
NC1=C2C(N([C@H]3CC[C@H](N4CCN(C)CC4)CC3)C=C2C5=CC=C(OC6=CC=CC=C6)C=C5)=NC=N1
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Synonyms
RK-20449
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (12)
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Journal Impact Factor
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Most Recent
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Blood
HCK is a survival determinant transactivated by mutated MYD88, and a direct target of ibrutinib. [Abstract]2016 Jun 23;127(25):3237-52. PMID: 27143257 -
Adv Sci (Weinh)
2025 Jun 30:e17764. PMID: 40586282 -
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J Med Chem
2024 Nov 28;67(22):20571-20579. PMID: 39513680 -
Commun Biol
Enhancing reprogramming towards induced human expanded pluripotency through substitution of SOX2 with engineered SOX17 transcription factors. [Abstract]2026 Apr 9;9(1):780. PMID: 41957290 -
Microb Pathog
Upregulation of haematopoetic cell kinase (Hck) activity by a secreted parasite effector protein (Ta9) drives proliferation of Theileria annulata-transformed leukocytes. [Abstract]2025 Feb:199:107252. PMID: 39730099 -
Biochem Biophys Res Commun
Hematopoietic cell kinase activation in skeletal myocytes contributes to local inflammation and pain sensitization in myofascial trigger points. [Abstract]2026 Aug 27:828:154112. PMID: 42269276 -
Res Sq
Cyclin-Dependent Kinase 5 Contributes to Bruton's Tyrosine Kinase Inhibitor Resistance via the IRE1α/XBP1 Axis in Mantle Cell Lymphoma. [Abstract]2026 May 8:rs.3.rs-9500406. PMID: 42147166 -
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Solvent & Solubility
In Vitro:
DMSO : 12.5 mg/mL (25.90 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.25 mg/mL (2.59 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.25 mg/mL (2.59 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
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Data Sheet (281 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Wilson MB, et al. Selective pyrrolo-pyrimidine inhibitors reveal a necessary role for Src family kinases in Bcr-Abl signal transduction and oncogenesis. Oncogene. 2002 Nov 21;21(53):8075-88. [Content Brief]
[2]. Zhang X, et al. Src-family tyrosine kinase activities are essential for differentiation of human embryonic stem cells. Stem Cell Res. 2014 Nov;13(3 Pt A):379-89. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0720 mL | 10.3599 mL | 20.7198 mL | 51.7995 mL |
| 5 mM | 0.4144 mL | 2.0720 mL | 4.1440 mL | 10.3599 mL | |
| 10 mM | 0.2072 mL | 1.0360 mL | 2.0720 mL | 5.1800 mL | |
| 15 mM | 0.1381 mL | 0.6907 mL | 1.3813 mL | 3.4533 mL | |
| 20 mM | 0.1036 mL | 0.5180 mL | 1.0360 mL | 2.5900 mL | |
| 25 mM | 0.0829 mL | 0.4144 mL | 0.8288 mL | 2.0720 mL |
A 419259 Related Classifications
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